Pressionorm,Helopharm,W. Germany,1981
Gepefrine is an orally active pressor agent and sympathomimetic agent. Gepefrine improves the early orthostatic disregulation of the arterial pressure[1][2][3].
Hydrolysis of D-(+)-1-(3-rnethoxyphenyl)-2-aminopropane: 2.42 mols (40 g)
of the compound are dissolved in 6N hydrochloric acid in a bomb tube
consisting of stainless steel and having a capacity of 500 ml. Hydrogen
chloride gas is passed into the ice-cooled solution until this is saturated, The
solution is then heated to 130°C for 2 hours in an air bath. After cooling and
driving off the hydrochloric acid at a slightly elevated temperature, the
hydrochloride of the 3-hydroxyphenyl derivative is present in the form of a
yellowish syrup.
The free base can be liberated from the hydrochloride by extracting a butanol
solution of the hydrochloride several times with sodium bicarbonate solution.
After recrystallization from isopropanol/ligroin, the yield of D-(+)-1-(3-
hydroxyphenyl)-2-aminopropane amounts to 33.0 g, corresponding to 90.1%
of theory relative to the D-form. Melting point = 152°C to 154°C.
[1] Peters FT, et al. Drug testing in blood: validated negative-ion chemical ionization gas chromatographic-mass spectrometric assay for determination of amphetamine and methamphetamine enantiomers and its application to toxicology cases. Clin Chem. 2002 Sep;48(9):1472-85. PMID:12194924
[2] Lossnitzer K, et al. Vergleichende Untersuchungen antihypotensiv wirksamer Sympathikomimetika im Kipptisch-Versuch [Therapy of orthostatic dysregulation. Comparative studies on anti-hypotensive sympathomimetics with a tilt-table test]. Fortschr Med. 1980 Aug 7;98(29):(1133-6). German. PMID:6108908
[3] Bachour G, et al. [Therapy of orthostatic dysregulation with gepefrin. Study with continuous telemetric blood pressure monitoring]. Z Kardiol. 1985 Apr;74(4):228-33. German. PMID:4002776
